IRA values calculated from the simulated agonist concentration-response curves shown in Fig. 3B
| Agonist | KD | Intrinsic efficacy | Relative activity6-a | EC50 | Emax6-b | Hill coefficient | Relative potency6-c | IRA6-d | CorrectedIRA6-e |
|---|---|---|---|---|---|---|---|---|---|
| μM | ɛ | μM | % | ||||||
| Standard agonist | 1.0 | 10 | 1.0 | 0.111 | 100 | 1.80 | 1.00 | 1.0 | |
| Agonist A | 1.0 | 5 | 0.5 | 0.243 | 96.9 | 1.67 | 0.457 | 0.443 | 0.5 |
| Agonist B | 1.0 | 2.5 | 0.25 | 0.554 | 86.7 | 1.49 | 0.200 | 0.174 | 0.25 |
| Agonist C | 1.0 | 1.25 | 0.125 | 1.17 | 61.2 | 1.34 | 0.0945 | 0.0583 | 0.125 |
| Agonist D | 1.0 | 0.6 | 0.06 | 1.92 | 26.6 | 1.26 | 0.0578 | 0.0153 | 0.060 |
| Agonist E | 1.0 | 0.3 | 0.03 | 2.31 | 8.29 | 1.23 | 0.0481 | 0.00399 | 0.030 |
| Agonist F | 1.0 | 0.15 | 0.015 | 2.43 | 2.18 | 1.22 | 0.0457 | 0.000996 | 0.015 |
The simulations were for a cooperative stimulus-response function (n = 2) with low sensitivity (K = 1.0) (see eq. 3).
↵6-a Relative activity is calculated from the dissociation constant (K D) and intrinsic efficacy (ɛ) using eq.5.
↵6-b The maximal response is expressed relative to that of the standard agonist.
↵6-c Denotes the EC50 value of the standard agonist divided by that of the test agonist.
↵6-d The IRA value was calculated from the EC50 and E max values according to eq.1.
↵6-e The corrected IRA values were calculated according to the method outlined in the .